Brefeldin A derivatives

Cytotoxic Michael addition derivatives of brefeldin A are described. Oxidation of thiol addition products of brefeldin A provides the corresponding sulfoxides and sulfones. The sulfoxides exhibited more cytotoxic activity than the corresponding sulfides and sulfones in a variety of human cancer cell...

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Bibliographische Detailangaben
Hauptverfasser: ARGADE ANKUSH B, DEVRAJ RAJESH, CUSHMAN MARK S, HAUGWITZ RUDIGER D
Format: Patent
Sprache:eng
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Zusammenfassung:Cytotoxic Michael addition derivatives of brefeldin A are described. Oxidation of thiol addition products of brefeldin A provides the corresponding sulfoxides and sulfones. The sulfoxides exhibited more cytotoxic activity than the corresponding sulfides and sulfones in a variety of human cancer cell lines. Pharmaceutical formulations of the disclosed cytotoxic derivatives are also described.